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CHRM5 Membrane Protein Introduction

Introduction of CHRM5

CHRM5, encoded by CHRM5 gene, is a member of G protein-coupled receptors family which has seven distinctive transmembrane domains. It is one of five subtypes of muscarinic receptors, M1-M5, widely expressed on the numerous cell types in the central nervous system. It has been shown that muscarinic receptors are the promising treatment targets for a number of pathological conditions of the central nervous system.

Basic Information of CHRM5
Protein Name muscarinic acetylcholine receptor M5
Gene Name CHRM5
Aliases HM5, M5R
Organism Homo sapiens (Human)
UniProt ID P08912
Transmembrane Times 7
Length (aa) 532
Sequence MEGDSYHNATTVNGTPVNHQPLERHRLWEVITIAAVTAVVSLITIVGNVLVMISFKVNSQ
LKTVNNYYLLSLACADLIIGIFSMNLYTTYILMGRWALGSLACDLWLALDYVASNASVMN
LLVISFDRYFSITRPLTYRAKRTPKRAGIMIGLAWLISFILWAPAILCWQYLVGKRTVPL
DECQIQFLSEPTITFGTAIAAFYIPVSVMTILYCRIYRETEKRTKDLADLQGSDSVTKAE
KRKPAHRALFRSCLRCPRPTLAQRERNQASWSSSRRSTSTTGKPSQATGPSANWAKAEQL
TTCSSYPSSEDEDKPATDPVLQVVYKSQGKESPGEEFSAEETEETFVKAETEKSDYDTPN
YLLSPAAAHRPKSQKCVAYKFRLVVKADGNQETNNGCHKVKIMPCPFPVAKEPSTKGLNP
NPSHQMTKRKRVVLVKERKAAQTLSAILLAFIITWTPYNIMVLVSTFCDKCVPVTLWHLG
YWLCYVNSTVNPICYALCNRTFRKTFKMLLLCRWKKKKVEEKLYWQGNSKLP

Function of CHRM5 Membrane Protein

CHRM5 can couple to Gq protein and mediate many of the diverse actions of acetylcholine in the central nervous system (CNS), as well as throughout non-nervous tissues innervated by the parasympathetic nervous system. The activation of M5 receptor activates phospholipase C, leading to release of calcium from the endoplasmic reticulum via the regulation of inositol trisphosphate and to activate protein kinase C by the mediation of diacylglycerol. In rodents, CHRM5 is important for prolonged dopamine release which is associated with schizophrenia. And it has been revealed that polymorphisms in CHRM5 gene combined with the alpha7-nicotinic receptor (CHRNA7) gene may be linked to schizophrenia. Moreover, CHRM5 upregulates in human lymphocytes during immunological responses which suggest that it may be involved in immune response. Additionally, like other subtypes of muscarinic receptors, M5 receptor also can be regarded as a therapeutic target for treating neurodegenerative disorders.

The structure and signaling pathways of muscarinic and nicotinic acetylcholine receptors. Fig.1 The structure and signaling pathways of muscarinic and nicotinic acetylcholine receptors. (Jones, 2012)

Application of CHRM5 Membrane Protein in Literature

  1. Berizzi A E., et al. Muscarinic M5 receptors modulate ethanol seeking in rats. Neuropsychopharmacology. 2018, 43(7): 1510-7. PubMed ID: 29483658

    The study reveals that ML375, a selective negative M5 muscarinic acetylcholine receptor allosteric modulator in rat, inhibits ethanol self-administration and decreases cue-induced reinstatement of ethanol seeking in ethanol-preferring (iP) rats. This suggests that M5 muscarinic acetylcholine receptor is a potential drug target for treating alcohol use disorders (AUDs).

  2. Deckmann K., et al. Muscarinic receptors 2 and 5 regulate bitter response of urethral brush cells via negative feedback. Faseb Journal. 2018, 32(6): 2903-10. PubMed ID: 29401598

    It is reported that a cholinergic chemosensory cell in the urethral epithelium and urethral brush cell is identified and it activates a reflex detrusor under stimulation with bitter or bacterial substances. The study reveals that muscarinic receptors 2 and 5 can reduce bitter response of urethral brush cell through a negative autocrine feedback mechanism. Moreover, muscarinic receptors 5 dysfunctions may generate bladder overactivity.

  3. Monica F., et al. Heat shock protein (Hsp) regulation by muscarinic acetylcholine receptor (mAChR) activation in the rat hippocampus. Journal of Cellular Physiology. 2018, 233(8): 6107-6116. PubMed ID: 29323700

    The study indicates that the activation of muscarinic acetylcholine receptor may be associated with the treatment of neurodegenerative disorders correlated with protein aggregation, such as Alzheimer disease.

  4. Gunter B W., et al. Selective inhibition of M5 muscarinic acetylcholine receptors attenuates cocaine self-administration in rats. Addiction Biology. 2017, 136(Pt C): 362-373. PubMed ID: 29138080

    The research firstly indicates that the selective inhibition of muscarinic receptors 5, M5 NAM ML375, can reduce both the reinforcing effects and the relative strength of cocaine. This suggests that M5 NAMs may be considered as a potential therapeutic target for treatment cocaine use disorder (CUD).

  5. Radu B M., et al. All muscarinic acetylcholine receptors (M1-M5) are expressed in murine brain microvascular endothelium. Scientific Reports. 2017, 7(1): 5083. PubMed ID: 28698560

    This article shows the expression of all muscarinic acetylcholine receptors (M1-M5) in mouse brain microvascular endothelium. M2, M3, and M5 expression are related to their respective protein levels, but no relationship between M1 and M4 expression and protein levels. Besides, acetylcholine with muscarinic receptors activates calcium transients in brain endothelium.

CHRM5 Preparation Options

To obtain the soluble and functional target protein, the versatile Magic™ membrane protein production platform in Creative Biolabs enables many flexible options, from which you can always find a better match for your particular project. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-CHRM5 antibody development services.


As a forward-looking research institute as well as a leading custom service provider in the field of membrane protein, Creative Biolabs has won good reputation among our worldwide customers for successfully accomplishing numerous challenging projects including generation of many functional membrane proteins. Please feel free to contact us for more information.

Reference

  1. Jones C K, et al. (2012). Muscarinic and nicotinic acetylcholine receptor agonists and allosteric modulators for the treatment of schizophrenia. Neuropsychopharmacology. 37(1): 16.

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